2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.

Topoisomerase Isoform Specific Products:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W654130
    Daunorubicin-13C,d3
    		Inhibitor
    Daunorubicin-13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin-<sup>13</sup>C,d<sub>3</sub>
  • HY-125580
    Makaluvamine A
    		Inhibitor
    Makaluvamine A is a member of Makaluvamines. Makaluvamines can be isolated from Fijian sponges of the genus Zyzzya, and possess inhibitory activity toward topoisomerase II along with cytotoxic activity against HCT-116 human colon cancer cells.
    Makaluvamine A
  • HY-13062R
    Daunorubicin (hydrochloride) (Standard)
    		Inhibitor
    Daunorubicin (hydrochloride) (Standard) is the analytical standard of Daunorubicin (hydrochloride). This product is intended for research and analytical applications. Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin (hydrochloride) (Standard)
  • HY-117543
    Ethonafide
    		Inhibitor
    Ethonafide (AMP-53) is an anthracene-containing derivative of Amonafide that belongs to the Azonafide series of anticancer agents. Ethonafide (AMP-53) inhibits topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIα and β.
    Ethonafide
  • HY-16742BR
    Gepotidacin (mesylate hydrate) (Standard)
    		Inhibitor
    Niacin (Standard) is the analytical standard of Niacin. This product is intended for research and analytical applications. Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases.
    Gepotidacin (mesylate hydrate) (Standard)
  • HY-125033S1
    EIDD-1931-d2
    EIDD-1931-d2 is the deuterium labeled 3,6-Dichloro-2-methoxybenzoic acid.
    EIDD-1931-d<sub>2</sub>
  • HY-108352
    HU 331
    		Inhibitor
    HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo.
    HU 331
  • HY-17381R
    Idarubicin (hydrochloride) (Standard)
    		Inhibitor
    Idarubicin (hydrochloride) (Standard) is the analytical standard of Idarubicin (hydrochloride). This product is intended for research and analytical applications. Idarubicin hydrochloride is an anthracycline antileukemic agent. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts.
    Idarubicin (hydrochloride) (Standard)
  • HY-13502AR
    Mitoxantrone (dihydrochloride) (Standard)
    		Inhibitor
    Mitoxantrone (dihydrochloride) (Standard) is the analytical standard of Mitoxantrone (dihydrochloride). This product is intended for research and analytical applications. Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone (dihydrochloride) (Standard)
  • HY-106307
    Retelliptine
    		Inhibitor
    Retelliptine (BD84), a derivative of ellipticine, is an inhibitor of Topoisomerase II with anticancer activity. Retelliptine can bind to DNA and inhibit Topoisomerase II during DNA replication.
    Retelliptine
  • HY-10581R
    Gatifloxacin (Standard)
    		Inhibitor
    Gatifloxacin (Standard) is the analytical standard of Gatifloxacin. This product is intended for research and analytical applications. Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin (Standard)
  • HY-A0170R
    Trovafloxacin (Standard)
    		Inhibitor
    Trovafloxacin (Standard) is the analytical standard of Trovafloxacin. This product is intended for research and analytical applications. Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
    Trovafloxacin (Standard)
  • HY-164271
    10-Boc-SN-38
    		Inhibitor
    10-Boc-SN-38 is a tert-butyloxycarbonyl (Boc)-protected form of SN-38 (HY-13704). SN-38 is the active metabolite of Irinotecan (HY-16562).
    10-Boc-SN-38
  • HY-156462
    Topoisomerase I inhibitor 9
    		Inhibitor
    Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM.
    Topoisomerase I inhibitor 9
  • HY-W653896
    Alternariol-d2
    		Inhibitor
    Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol-d<sub>2</sub>
  • HY-N0716
    Berberine
    		Inhibitor
    Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. The sulfate form (HY-N0716B) improves bioavailability.
    Berberine
  • HY-10919
    C-1311
    		Inhibitor
    C-1311 shows to inhibit the catalytic activity of DNA topoisomerase II in vitro and in tumour cells. C-1311 prolongs G2 arrest followed by G2 to M transit and cell death during mitosis in the process of mitotic catastrophe.
    C-1311
  • HY-118726
    Luotonin F
    		Inhibitor
    Luotonin F is an alkaloid found in the aerial parts of the P. nigellastrum Bunge. Luotonin F shows cytotoxic activity against mouse leukemia P-388 cells by inhibiting human topoisomerase II.
    Luotonin F
  • HY-118379
    NU/ICRF 500
    		Inhibitor
    NU/ICRF 500 is a topo II catalytic inhibitor which increases CREST negative micronuclei in human lymphocytes.
    NU/ICRF 500
  • HY-16742B
    Gepotidacin mesylate hydrate
    		Inhibitor 99.62%
    Gepotidacin mesylate hydrate is an orally active triazaacenaphthylene antibiotic and bacterial type II topoisomerase inhibitor. Gepotidacin mesylate hydrate inhibits bacterial DNA replication by blocking topoisomerase enzymes. Gepotidacin mesylate hydrate selectively inhibits topoisomerase IV and the B subunit of DNA gyrase.
    Gepotidacin mesylate hydrate
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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